First case of Dolutegravir and Darunavir/r multi drug-resistant HIV-1 in Cameroon following exposure to Raltegravir: lessons and implications in the era of transition to Dolutegravir-based regimens.
PMID: 32843050
2020
Antimicrobial resistance and infection control
Conclusion: Detected RAMs were M41L, K70Q, V75I, Q151M, M184V and T215F for NRTI; K103N and V108I for NNRTI; and L10F, K20I, M36I, M46I, I47V, I54L, L63H, L76V, V82S and L89I for PI/r.
Detection of human immunodeficiency virus type 1 transmitted drug resistance among treatment-naive individuals residing in Jakarta, Indonesia.
Abstract: Drug resistance-related major mutation was not detected in protease fragments of pol gene, but two major mutations, K103N (6.67%) and Y181C (6.67%), were detected in reverse transcriptase fragments of pol gene.
Conclusion: The drug resistance-associated major mutations, K103N (6.67%) and Y181C (7.14%), were detected in RT genes, suggesting the emergence of TDR in Jakarta.
Result: Two major mutations against NNRTIs, K103N and Y181C, were detected in peripheral blood samples derived from 2 patients, SS21 and SS41 (Table 1).
Discussion: ART e
New indolylarylsulfone non-nucleoside reverse transcriptase inhibitors show low nanomolar inhibition of single and double HIV-1 mutant strains.
PMID: 32883642
2020
European journal of medicinal chemistry
Abstract: Among these, IAS 12 exhibited a remarkable antiviral activity against single and double mutants (K103N EC50 = <0.7 nM; Y181C EC50 = <0.7 nM; Y188L EC50 = 21.3 nM; K103N-Y181C EC50 = 6.2 nM), resulting equally or more active than previuosly reported IAS 6 and some approved anti-HIV-1 drugs.
Abstract: Docking and molecular dynamics simulations of compound 12 in complex with WT, Y181C, Y188L, K103N and K103N-Y181C RTs clarified a general binding mode that was consistent with biological results.
Abstract: Kinetic experiments disclosed that derivative 12 preferentially binds WT and
Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.
PMID: 32925358
2020
Journal of acquired immune deficiency syndromes (1999)
Abstract: DOR was rationally designed to address limitations associated with other approved NNRTIs, particularly resistance from common NNRTI resistance-associated mutants containing K103N, Y181C, or G190A reverse transcriptase substitutions.
Introduction: B
Method: None of these participants had RT K103N, Y181C, or G190A substitutions at baseline.
Method: Overall, 4% (n = 24/656) of participants entered the trial with RT K103N, Y181C, and/or G190A substitutions.
Drug Resistance Spread in 6 Metropolitan Regions, Germany, 2001-2018(1).
Abstract: Phylogenetic and network analysis elucidated numerous cases of shared drug resistance mutations among genetically linked patients; K103N was the most frequently shared mutation.
Patterns of acquired HIV-1 drug resistance mutations and predictors of virological failure in Moshi, Northern Tanzania.
Abstract: Frequent NNRTI-resistance associated mutations were K103N (n = 11), V106M (n = 5) and G190A (n = 5).
Result: The most frequent NNRTI resistance-associated mutations were K103N (44%), V106M (20%), and G190A (20%) (Fig 3), all of these three mutations confer high-level resistance to efavirenz and nevirapine.
Table: K103N
Discussion: The most frequent NNRTI resistance-associated mutations were K103N, V106M, and G190A that confer high-level resistance to efavirenz and nevirapine.
Increased HIV-1 pretreatment drug resistance with consistent clade homogeneity among ART-naive HIV-1 infected individuals in Ethiopia.
Abstract: The most frequently observed NNRTIs-associated mutations common to both algorithms were
Result: Both CPR tool and IAS-USA algorithms were concordant in identifying five NNRTIs resistance-associated mutations: K103N in one patient (1.96%), Y188L, and H221Y in another patient (1.96%), K101E in one patient (1.96%), and V106A in another patient (1.96%).
Table: K103N
Discussion: In agreement with our report, K101E, K103N, and E138A mutations of the RT region had been reported previously in Ethiopia among ART-naive individuals.
Virologic suppression in patients with a documented M184V/I mutation based on the number of active agents in the antiretroviral regimen.
Abstract: Over the past 40 years, the frequency of the DRM M184V (50-64.3%, p=0.363), G190A (17.2-46.2%, p=0.021), and K103N (34.5-42.3%, p=0.551) increased, while the frequency of Y181C (17.2-7.7%, p=0.289) decreased.
Abstract: The major DRM in the NRTIs was the M184V, whereas the G190A, K103N, and Y181C were the major DRMs in the NNRTIs.
Transmitted and Acquired HIV-1 Drug Resistance from a Family: A Case Study.
Abstract: Mother also acquired K101E (41.03%), K103N (27.56%) and minor mutation of V106M (4.30%) after improperly discontinuing antiretroviral regimen of lamivudine (3TC), tenofovir (TDF) and efavirenz (EFV).
Introduction: A major disadvantage of EFV is the low genetic barrier that certain single amino acid mutation, such as K103N, V106M, can cause a high level of drug resistance.
Result: However, for patient M, V106M alone is associated with a high-level reduction in NVP (60) and EFV (60) susceptibility as well as an intermediate reduction in DOR (50) susceptibility, while together with V106I, especially K101E and K1
HIV mutation literature information.
PMID: 
2020
Antimicrobial resistance and infection control
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